[Translation] A single-center, open-label, single-dose clinical trial evaluating the absorption, metabolism, and excretion of 3 mg/100 μCi [14C] azithromycin suspension in healthy male subjects

主要目的： 1 考察[14C]标记的阿兹夫定在健康男性受试者全血和血浆中总放射性的药代动力学特征； 2 定量分析健康男性受试者口服[14C]阿兹夫定混悬液后呼出气体与排泄物中总放射性，获得人体内物质平衡数据，确定主要排泄途径；次要目的： 1 定量分析血浆中阿兹夫定原形药物及代谢产物（如适用）浓度，获得血浆中阿兹夫定的药代动力学参数； 2 观察单剂量口服 [14C]阿兹夫定混悬剂后受试者的安全性。探索性目的： 1 测定健康男性受试者口服[14C]阿兹夫定后血浆、尿液和粪便中的放射性代谢物谱，并鉴定主要代谢产物，提供阿兹夫定在人体内的主要代谢途径数据，确定主要生物转化途径。 2 测定健康男性受试者口服[14C]阿兹夫定混悬液后，细胞内的分布情况。

[Translation]

Main objectives: 1 To investigate the pharmacokinetic characteristics of total radioactivity of [14C]-labeled azithromycin in whole blood and plasma of healthy male subjects; 2 To quantitatively analyze the total radioactivity in exhaled gas and excreta of healthy male subjects after oral administration of [14C]azithromycin suspension, obtain material balance data in the human body, and determine the main excretion pathway; Secondary objectives: 1 To quantitatively analyze the concentration of parent drug and metabolites (if applicable) in plasma of azithromycin and obtain the pharmacokinetic parameters of azithromycin in plasma; 2 To observe the safety of subjects after a single oral dose of [14C]azithromycin suspension. Exploratory objectives: 1 To determine the radioactive metabolite spectrum in plasma, urine and feces of healthy male subjects after oral administration of [14C]azithromycin, and identify the main metabolites, provide data on the main metabolic pathways of azithromycin in the human body, and determine the main biotransformation pathways. 2 To determine the intracellular distribution of [14C]azithromycin suspension in healthy male subjects after oral administration.

Start Date18 Jul 2024

Sponsor / Collaborator

Beijing Union Pharmaceutical Factory

[+1]

NCT06349655

/ CompletedNot ApplicableIIT

Real-World Effectiveness and Safety of Oral Azvudine in Hospitalized Patients With COVID-19: A Multicenter, Retrospective, Cohort Study

To establish a real-world clinical cohort and database of Azvudine in the treatment of SARS-CoV-2 infection, and to provide stable and reliable evidence for the clinical efficacy and safety evaluation of azvudine in the treatment of SARS-CoV-2 infection.

Start Date05 Dec 2023

Sponsor / Collaborator

The First Affiliated Hospital of Zhengzhou University

[+1]

100 Clinical Results associated with RT x RdRp

100 Translational Medicine associated with RT x RdRp

0 Patents (Medical) associated with RT x RdRp

Literatures (Medical) associated with RT x RdRp

01 Mar 2023·European Journal of Medicinal Chemistry

Recent advances on dual inhibitors targeting HIV reverse transcriptase associated polymerase and ribonuclease H

Review

Author: Zhao, Guang-Kuan ; Yang, Xiu-Ming ; Kang, Jia-Xiong ; Huang, Mou-Xin ; Ouyang, Qin ; Zeng, Rong ; Hui, Wen-Qi

Reverse transcriptase (RT) plays an indispensable role in the replication of human immunodeficiency virus (HIV) through its associated polymerase and ribonuclease H (RNase H) activities during the viral RNA genome transformation into proviral DNA. Due to the fact that HIV is a highly mutagenic virus and easily resistant to single-target RT inhibitors, dual inhibitors targeting HIV RT associated polymerase and RNase H have been developed. These dual inhibitors have the advantages of increasing efficacy, reducing drug resistance, drug-drug interactions, and cytotoxicity, as well as improving patient compliance. In this review, we summarize recent advances in polymerase/RNase H dual inhibitors focusing on drug design strategies, and structure-activity relationships and share new insights into developing anti-HIV drugs.

01 Aug 2022·Infectious Disorders - Drug Targets

A Review on the New Indication of Nucleoside Reverse Transcriptase Inhibitors (NRTIs) in the Treatment of Coronavirus Disease 2019

Review

Author: Hosseinjani, Hesamoddin ; Salari, Sofia ; Karbasforooshan, Hedyieh

Background:In December 2019, a new coronavirus (nCoV) emerged as a public health concern spreading all around the world. Several attempts have been made to discover effective drugs and vaccines. Up to now, multiple COVID-19 vaccines have been developed against this mysterious virus, and a lot of individuals have already got vaccinated.Objective:Anti-viral drugs are effective in treating and managing COVID-19. Nucleoside reverse transcriptase inhibitors (NRTIs) are a collection of antiviral drugs for treating HIV and HBV infections. These drugs prevent virus replication by blocking reverse transcriptase (RT). In this review, we discuss the interaction of this class of anti- HIV drugs with specific functional proteins and enzymes of SARSCoV- 2.Method:A search of the databases, including Web of Science, Embase, PubMed, Scopus, and Google Scholar, was conducted from commencement to September 2020. The relevant articles on the potential effects of NRTIs on COVID-19 were collected. Finally, twenty-three articles were selected, including all in vitro, in vivo, and clinical studies.Result:It was observed that RdRp, spike, ACE2, PNP, inflammatory cytokines, and nucleocapsid protein participate in the pathogenesis of SARS-CoV-2. NRTIs target these proteins by binding to them.Conclusion:This review is focused on the mechanisms of NRTIs to introduce them as potential therapies for COVID-19. However, further in vitro and in vivo investigations will provide helpful information for the identification of drug candidates as a part of COVID-19 management.

27 Oct 2021·Molecular Biology and Evolution

RdRp or RT, That is the Question

Article

Author: Peyambari, Mahtab ; Guan, Shengxi ; Roossinck, Marilyn J

AbstractThe RNA-dependent RNA polymerase (RdRp) of all known double-stranded RNA viruses is located within the viral particle and is responsible for the transcription and replication of the viral genome. Through an RT-PCR assay, we determined that purified virions, in vitro translated RdRp proteins, and purified recombinant RdRp proteins of partitiviruses also have reverse transcriptase (RT) function. We show that partitivirus RdRps 1) synthesized DNA from homologous and heterologous dsRNA templates; 2) are active using both ssRNA and dsRNA templates; and 3) are active at lower temperatures compared to an optimal reaction temperature of commercial RT enzymes. This finding poses an intriguing question: why do partitiviruses, with dsRNA genomes, have a polymerase with RT functions? In comparison, 3Dpol, the RdRp of poliovirus, did not show any RT activity. Our findings lead us to propose a new evolutionary model for RNA viruses where the RdRp of dsRNA viruses could be the ancestor of RdRps.

Analysis

Perform a panoramic analysis of this field.

view full example data

AI Agents Built for Biopharma Breakthroughs

Accelerate discovery. Empower decisions. Transform outcomes.

Get started for free today!

Accelerate Strategic R&D decision making with Synapse, PatSnap’s AI-powered Connected Innovation Intelligence Platform Built for Life Sciences Professionals.

Start your data trial now!

Synapse data is also accessible to external entities via APIs or data packages. Empower better decisions with the latest in pharmaceutical intelligence.

Bio

Bio Sequences Search & Analysis

Chemical

Chemical Structures Search & Analysis